C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 417/06 (2006.01) A61K 31/365 (2006.01) A61K 31/427 (2006.01) A61K 31/4427 (2006.01) A61P 35/02 (2006.01) C07D 303/00 (2006.01) C07D 313/00 (2006.01) C07D 405/06 (2006.01) C07D 407/06 (2006.01) C07D 493/04 (2006.01)
Patent
CA 2456280
The invention relates to cis- and trans-12, 13-cyclopropyl and 12, 13- cyclobutyl epothilones of formula (I) to (IV), wherein Ar is a radical represented by the following structure:, and the other radicals and symbols have the meanings as defined herein; to their chemical synthesis and biological evaluation; their use in the treatment of neoplastic diseases and to pharmaceutical preparations containing such compounds. The compounds described herein are potent tubulin polymerization promoters and cytotoxic agents.
L'invention concerne des cis- et trans-12, 13-cyclopropyl et 12, 13-cyclobutyl épothilones représentés par les formules I à IV, Ar étant un radical représenté par la structure A, les autres radicaux et symboles ayant les significations telles que définies ci-après, ainsi que leur synthèse chimique et leur évaluation biologique, leur utilisation dans le traitement des maladies néoplastiques et des préparations pharmaceutiques contenant ces composés. Les composés susmentionnés sont des promoteurs puissants de la polymérisation de la tubuline et des agents cytotoxiques.
Altmann Karl-Heinz
Namoto Kenji
Nicolaou Kyriacos Costa
Ritzen Andreas
Shoji Mutsuru
Fetherstonhaugh & Co.
Novartis Ag
The Scripps Research Institute
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